Abstract:
The ion exchange adriamycin carboxymethyl-dextran-microspheres (AD-CMDMS) was chosen as a model preparation. Pharmacokinetics, targeting and embolization effects of the microspheres were studies after hepatic arterial embolization in vitro in dogs.After hepatic arterial infusion, the concentrations of ADM in peripheral vein blood and hepatic tissue were determined by HPLC. The peak concentrations were (0.558 μg/ml for AD-CM-DMS and 1.013 μg/ml for ADM solution.
T1/2 (α),
T1/2 (β) and MRT of AD-CM-DMS were respectively 2.82, 3. 19 and 1.28 times as much as those of ADM solution. At the target site, the tissue concentrations of AD-CM-DMS were respectively 8.0 and 9.1 times those of ADM solution. The dynamic vessel angiography revealed no external and internal collaterals and no complete degradation of ADCM-DMS after sixteen weeks was observed. These results suggest that AD-CM-DMS are useful as embolic agent for the treatment of hepatic career. It could facilitate intensive chemotherapy with minimum systematic side effect.